Drug intelligence / Profile preview

SK1-I

Development stage
Preclinical
Lead developer
Enzo Biochem
Modality
Small Molecules
Administration
Unknown
01

Overview

SK1-I is a **small molecule inhibitor** that selectively and competitively inhibits **sphingosine kinase 1** (SK1), with a Ki value of 10 μM. It is an analog of sphingosine and does not inhibit sphingosine kinase 2 or other kinases such as PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ, or CamK2β. SK1-I decreases sphingosine-1-phosphate (S1P) levels and causes accumulation of proapoptotic ceramide, exhibiting antiproliferative properties and inhibiting tumor growth in vitro and in vivo. Preclinical studies have shown potential in cancer and autoimmune disease models[1][3][5][7][13][16].

Other names
(2R,3S,4E)-N-methyl-5-(4′-pentylphenyl)-2-aminopent-4-ene-1,3-diolBML-258 hydrochlorideBML258 hydrochlorideBML 258 hydrochloride
02

Targets

SPHK1 (Sphingosine kinase 1)

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